1. GPCR/G Protein
    Neuronal Signaling
  2. Adrenergic Receptor
  3. Nebivolol

Nebivolol (Synonyms: R 065824)

Cat. No.: HY-B0203
Handling Instructions

Nebivolol selectively inhibits β1- adrenergic receptor with IC50 of 0.8 nM.

For research use only. We do not sell to patients.

Nebivolol Chemical Structure

Nebivolol Chemical Structure

CAS No. : 118457-14-0

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Description

Nebivolol selectively inhibits β1- adrenergic receptor with IC50 of 0.8 nM. Target: β1- adrenergic receptor Nebivolol reduces cell proliferation of human coronary smooth muscle cells (haCSMCs) and endothelial cells (haECs) in a concentration- and time-dependent maner. Nebivolol treatment for 7 days causes significant reduction in cell growth of haCSMCs with IC50 of 6.1 μM, and inhibits accelerated haCSMC proliferation stimulated by growth factors PDGF-BB, bFGF, and TGFβ with IC50 values of 6.8 μM, 6.4 μM and 7.7 μM, repectively. Nebivolol treatment (10-5 M) of haCSMCs for 48 hours induces a moderate apoptosis of 23% and a decrease from 16% to 5% in the number of cells in S-phase. During Nebivolol incubation, NO formation of HaCEs increases, while endothelin-1 transcription and secretion are suppressed. Administratiion of Nebivolol (initially by iv within 10 minutes of reperfusion and then orally) to rats with myocardial infarction (MI) reduces myocardial apoptosis, which is mediated by regulation of NO . Nebivolol, significantly, prevents left ventricular (LV) pressure changes, reduces total and regional apoptotic cardiomyocytes. Nebivolol treatment lowers mean blood pressure (MBP) in rats with MI slightly, but not significantly.

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Molecular Weight

405.44

Formula

C₂₂H₂₅F₂NO₄

CAS No.

118457-14-0

SMILES

FC1=CC=C2C(CC[[email protected]]([[email protected]@H](O)CNC[[email protected]](O)[[email protected]@]3([H])CCC(C=C(F)C=C4)=C4O3)([H])O2)=C1

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Keywords:

NebivololR 065824R065824R-065824Adrenergic ReceptorBeta ReceptorInhibitorinhibitorinhibit

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